Sunitinib Malate

Licensed by Pfizer Catalog No.S1042

Sunitinib Malate Chemical Structure

Molecular Weight(MW): 532.56

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.

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In DMSO USD 191 In stock
USD 97 In stock
USD 147 In stock
USD 447 In stock

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Cited by 42 Publications

11 Customer Reviews

  • PDGF-AA induces Ezh2 expression and proliferation in juvenile islets but not in adult islets. Western immunoblots of indicated islet proteins from 3 week or 9 month-old WT islets 2 days after exposure to PDGF-AA alone, or PDGF-AA plus RTK inhibitors Sunitinib.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

    Assessment of effects on human juvenile or adult islets after exposure to PDGF-AA (50 ng/ml) for 2 days, with or without Sunitinib (2 uM) or U0126 (10 uM)co-treatment. Average percentage of BrdU+ insulin+ cells was morphometry from sectioned islets immunostained for insulin (green), glucagon (white) and BrdU (red). n = 3-6 independent experiments.

    Nature 2011 478(7369):349-55. Sunitinib Malate purchased from Selleck.

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Sunitinib Malate purchased from Selleck.

    Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

  • Sunitinib or PD98059 decreases cell proliferation in a dose-dependent manner. H295R and SW13 cells were treated with various concentration of sunitinib or PD98059 for 48 hours as indicated. Treated cells were subjected to the MTS proliferation assay. Similar experiments were repeated 3 times. Histograms represent relative % of OD490 nm absorbance (* P < .05). All data are relative multiples of expression compared with untreated cells. The data are representative of three experiments and are expressed as the mean ?SE.

    Surgery 2012 152, 1045-50. Sunitinib Malate purchased from Selleck.

    Autophagic activation in sunitinib- and sorafenib- but not AZD6244-treated cells. Medullary thyroid cancer-1.1 (MTC-1.1; A) and TT ( B) cells were treated with dimethyl sulfoxide (DMSO), sunitinib (50 nM), sorafenib (10 nM), AZD6244 (30 nM), or everolimus (20 nM) for 48 hours. Cell lysates were prepared, and light chain 3 (LC3)-I and -II cleaved caspase-3 protein levels were monitored by Western blotting. Reprobing against actin was per formed to ensure equal protein loading. ( C ) MTC-1.1 and TT cells were transiently transfected with autophagy protein 5 (Atg-5) small inter fering RNA. Transfection with scrambled small inter fering RNA was used as a control. After transfection, cells with and without Atg-5 knockdown were exposed to DMSO or 20 nM of everolimus for 48 hours. Cell lysates were pre- pared and LC3-I and -II protein expression levels were monitored by Western blotting. Reprobing against Atg-5 was per formed to monitor Atg-5 knockdown efficiency. Reprobing against actin was per formed to ensure equal protein.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

  • Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error.

    Surgery 2012 152, 1142-9. Sunitinib Malate purchased from Selleck.

    Sunitinib limits the colonial growth of HT-29 by downregulating HIF-1a. (A) The number and size of colonies formed in soft agar. The numbers of small colonies (<50 μm diameter) were not different among conditions of a serial concentration of sunitinib. On the contrary, large colonies (>50 μm diameter) disappeared after incubation with sunitinib. Each point represents the mean and SD from four separate experiments. (B) HIF-1a expression and hypoxia within HT-29 colony. After colonies grew for 4 weeks, HIF-1a and hypoxia were visualized by immunofluoroscence staining. Bar = 20 μm.

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • 2. Sunitinib downregulates HIF-1a. (A) Dose-dependent repression of HIF-1a protein level by sunitinib in HT-29. HT-29 cells were incubated under normoxic (N) or hypoxic (H) conditions in the presence of sunitinib for 24 h. HIF-1a and ARNT proteins in total cell lysates were analyzed by Western blotting. (B) Sunitinib attenuates the hypoxic induction of HIF-1 target genes. RNAs were isolated from HT-29 cells subjected to normoxia (N) or hypoxia (H) in the presence of sunitinib for 16 h. The mRNAs of HIF-1a and its target genes were analyzed by RT-PCR and autoradiography. PGK1 indicates phosphoglycerate kinase 1; PDK1, pyruvate dyhydrogenase kinase 1; CAIX, carbonic anhydrase IX. (C) Sunitinib-induced HIF-1 inhibition. Epo-enhancer and b- galactosidase reporter plasmids were co-transfected into HEK293 cells. After 16 h incubation, luciferase and b-galactosidase activities were measured. *P < .05 versus the hypoxic control.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

    Sunitinib inhibits 50-UTR-dependent translation of HIF-1a. (A) 50 cap-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the tk promoter and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 lg per 100-mm dish) and the b-gal plasmid (4 μg). After 16 h incubation under normoxic or hypoxic conditions with sunitinib, cells were lysed and subjected to luciferase assay. *P < .05 versus the hypoxic control. (B) IRES-dependent translational activity of HIF-1a. The luciferase reporter plasmid contains the HIF-1a 50-UTR segment between the GFP gene and the luciferase gene. HT-29 cells were co-transfected with the reporter plasmid (8 μg) and the b-gal plasmid (4 μg). *P < .05 versus the hypoxic control. (C) Sunitinib inhibits phosphorylation of Akt. After 8 h incubation under hypoxic condition with sunitinib, HT-29 cells were lysed and subjected to Western blotting. (D) Sunitinib suppresses HIF-1a in VHL-null RCC4 cells. VHL (-/-) RCC4 cells were incubated under normoxic conditions sunitinib for 8 h, and HIF-1a in total cell lysates was analyzed by Western blotting.

     

     

    Biochem Bioph Res Co 2010 398, 205–211. Sunitinib Malate purchased from Selleck.

  • Experimental layout for VEGF signaling blocking and LCMV infection in WT mice. Mice received two injections on day 0 and 3 p.i. of Abs as described in Material and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib. Inguinal LN volume on day 0 (D0) or day 8 (D8) p.i. after treatment of mice with control Ig or anti-VEGFR2, anti-VEGF-A Abs or sunitinib. Pooled from 1-2 independent experiments with 3-5 mice per treatment. D. Total HEV length on day 0 (D0) or day 8 (D8) p.i. as in C. No significant difference was found in C and D between day 8 control Ig and Ab- or inhibitor-treated values (One-way ANOVA).

    AACR Sunitinib Malate purchased from Selleck.

Purity & Quality Control

Choose Selective PDGFR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
Targets
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
2 nM 80 nM 2.9 μM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 NG[3bHFMcW6jc3WgRZN{[Xl? M4fzbmlvcGmkaYTpc44hd2ZiUFTHSk1qdmS3Y3XkJGJz\FViaX7jc5Jxd3KjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFch|ryP MUmxNlY1PjBzOR?=
3T3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPT[IhKdmirYnn0bY9vKG:oIGDsZZRmdGW2LXTldol3\WRiZ4Lve5RpKG[jY4TvdkBqdmS3Y3XkJFNVOyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODFizszN MVmxNlY1PjBzOR?=
3T3 NVLrTWZ1TnWwY4Tpc44hSXO|YYm= NWm5S4pmUW6qaXLpeIlwdiCxZjDWZZNkfWyjcjDlcoRwfGinbHnhcEBoem:5dHig[oFkfG:{IILlZ4VxfG:{IIfpeIghUUN3MDDv[kAxNjB3IN88US=> MXmxNlY1PjBzOR?=
3T3 M1;tNGtqdmG|ZTDBd5NigQ>? NH7XbpUzOCCvaX6= NILrNnJFVVOR MVPD[YxtfWyjcjDpcohq[mm2aX;uJI9nKF[HR1[gbY5lfWOnZDDoeY1idiCNRGKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{MjFOwG0> NIi3OHgyPjF4MkCwPC=>
NIH3T3 M3rJVGtqdmG|ZTDBd5NigQ>? NYHzZVdmOjBibXnu NEGyWFlFVVOR M1Pn[IlvcGmkaYSgbJVu[W5iS1TSJItqdmG|ZTDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDBwMEG4JO69VQ>? NGDpeYEyPjF4MkCwPC=>
A549 M1PqRWZ2dmO2aX;uJGF{e2G7 MYDEUXNQ NYjReZFMUW6qaXLpeIlwdiCxZjDjMW1mfCCmZYDlcoRmdnRiSFfGMYlv\HWlZXSgbJVu[W5iQUW0PUBk\WyuIH3p[5JifGmxbjD3bZRpKEmFNUCgc4YhOiEQvF2= NYnmU5Q6OTh2M{SxOFU>
DU145 NFTJe5JHfW6ldHnvckBCe3OjeR?= NGjve2RFVVOR NXrHfXJpUW6qaXLpeIlwdiCxZjDjMW1mfCCmZYDlcoRmdnRiSFfGMYlv\HWlZXSgbJVu[W5iRGWxOFUh[2WubDDzZ4F1fGW{aX7nJJdqfGhiSVO1NEBw\iBzMDFOwG0> Mlj5NVg1OzRzNEW=
KB3-1 MVfDfZRwfG:6aXOgRZN{[Xl? MW[3NkBp NGjORnZFVVOR M2[5[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\3BvbnXnZZRqfmViS1KtN{0yKGOnbHzzJJdqfGhiSVO1NEBw\iB{LkOg{txO MUKxPVM6PzN{Mh?=
KBV1 NXPhWGhQS3m2b4TvfIlkKEG|c3H5 NFjzb5c4OiCq M{nHdWROW09? NWrXc5VmS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWC2pbInjc5Bzd3SnaX6t[ZhxemW|c3nu[{BMSlZzIHPlcIx{KHerdHigTWM2OCCxZjC0MlEh|ryP MWexPVM6PzN{Mh?=
A375 M3r6emN6fG:2b4jpZ{BCe3OjeR?= MlvFO|IhcA>? NFHE[G5FVVOR MXHJR|UxRTVwNDFOwG0> M{TzVVE6PjV2NEC4
RS4-11 MWLGeY5kfGmxbjDBd5NigQ>? MnW2NkBp MnzsTY5pcWKrdHnvckBw\iCITGSzJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFA6QSEQvF2= NH7WN5kyQTZ3NESwPC=>
RS4-11 NHnrOYRHfW6ldHnvckBCe3OjeR?= Ml\iNkBp NFvONGdKdmirYnn0bY9vKG:oIF\MWFMhUVSGIH31eIFvfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB|NDFOwG0> M4nTXVE6PjV2NEC4
Sf9 MVrLbY5ie2ViQYPzZZk> MV2zNEBucW5? MU\Jcohq[mm2aX;uJI9nKEeVVD30ZYdo\WRiVlXHSnIh\XiycnXzd4VlKHerdHigTWM2OCCxZjCwMlE5PSEQvF2= NHnZWYEyQTh3NEC1NS=>
Ba/F3 NVuxbow3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvMRlNzPzJiaB?= NUHOSlFqUUN3ME2xMlIh|ryP NUTVe4szOjBzMUewNFQ>
BaPTC2 M17NUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXjO3U3PzJiaB?= NYHEUmdwUUN3ME2wMlIzKM7:TR?= M4TZWVIxOTF5MEC0
Sf9 MmXNSpVv[3Srb36gRZN{[Xl? NUG0XIdkOSCq MoHQSG1UVw>? NIjtWXFKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IFjpd{11[WepZXSgVmVVKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNU4{KM7:TR?= MnzMNlAyOTdyMES=
H4 MmLVR5l1d3SxeHnjJGF{e2G7 NHu0dmEyOCEQvF2= NWfYSWk5XG:6aXPpeJkhcW5iaIXtZY4hUDRiY3XscJM> Mnu1NlA{PTB6ME[=
SF-539 NVHj[GJWU2mwYYPlJGF{e2G7 NGLXfoI{OzNizszN M2XLNFYxKG2rbh?= M{nPVWROW09? NFq1XpNKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFEzNjJizszN MkDBNlA1ODN5MEC=
U251 NFzuSHBMcW6jc3WgRZN{[Xl? Ml\ON|M{KM7:TR?= M2j4WVYxKG2rbh?= MV3EUXNQ NXjQWYM4UW6qaXLpeIlwdiCxZjDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxPE46KM7:TR?= MV[yNFQxOzdyMB?=
A431 M4\Db2tqdmG|ZTDBd5NigQ>? Mn62TY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyOi5{IN88US=> NGK3WYwzODV3OEC3Ni=>
A431 MVXLbY5ie2ViQYPzZZk> NYDLRlRvUW6qaXLpeIlwdiCxZjDWSWdHWjJiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyQC57IN88US=> M2rQNlIxPTV6MEey
HepG2 M4O3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T2NFczKGh? Mo\sTWM2OD1|LkixJO69VQ>? NIDQWVYzODV5MEWyOi=>
Kasumi-1 NUjF[2l6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\LR5ZwPzJiaB?= NYXjTJlmUUN3ME2wMlAyPiEQvF2= NE\kT5MzODV5MEWyOi=>
RS4-11 NX3EW|FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUe1cVBkPzJiaB?= MXXJR|UxRTFizszN NIXQWJQzODV5MEWyOi=>
THP1 M{H5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPofm0xPzJiaB?= M2XkeWlEPTB;MD61JO69VQ>? M4L3WFIxPTdyNUK2
Kasumi-1 NWnGVo5LTnWwY4Tpc44hSXO|YYm= MorXTY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAyPSEQvF2= NVLDb3lUOjB6M{OwN|k>
A549 M1TqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXFNVYhcA>? MoLPRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\Wyucx?= M33nVlIyPDVyNE[z
HL60 NHW4bFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXixOkBp MXnBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy| NWDMdlQxOjF2NUC0OlM>
HUVEC M3vxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjoNVYhcA>? MkPvTY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iB{Lke1JO69VQ>? MXmyNVQ2ODR4Mx?=
HUVEC NVTiS5RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\uc5VQOTZiaB?= NULDeZBuUW6qaXLpeIlwdiCxZjDiSmdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjC0MlA1KM7:TR?= M3\5U|IyPDVyNE[z
IM9 NFn4SlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnezNVYhcA>? M1r5eWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFnNPUBk\Wyucx?= NHGyfIszOTR3MES2Ny=>
K562 Ml3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrhNVYhcA>? NF\tfXNCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzz NY[1b5ZuOjF2NUC0OlM>
MDA-MB-231 Ml7kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j4OlE3KGh? NXixV5lwSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\Wyucx?= MnPDNlE1PTB2NkO=
H460 M2HaRmN6fG:2b4jpZ{BCe3OjeR?= NYPxdVlxPzJiaB?= NHu2TpVKSzVyPUKuO{DPxE1? M1Pqd|IyPjJzOEiw
SMMC7721 MVrDfZRwfG:6aXOgRZN{[Xl? MnjmO|IhcA>? NHvPOoVKSzVyPU[uOFch|ryP MmPSNlE3OjF6OEC=
WI38 Mle1R5l1d3SxeHnjJGF{e2G7 NUHUdmw{PzJiaB?= M3LVTWlEPTB;OD61OkDPxE1? M2nDUVIyPjJzOEiw
HEK293 MX;LbY5ie2ViQYPzZZk> NI\WWXEyODBibl2= M33LfVEhcA>? MlLO[I9meyCwb4SgbY5pcWKrdDDWSWdHNWmwZIXj[YQh[XW2b4Doc5NxcG:{eXzheIlwdiCxZjD0fZJwe2mwZTCxNVc2KHKnc3nkeYUhd25iVlXHSnIzKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJM> MV[yNVg5PTJ6Nx?=
HUVEC NI[1WoFHfW6ldHnvckBCe3OjeR?= NIPzWIoyKM7:TR?= NUfH[XVGOjRiaB?= M3X5bGFvfGmjbnfpc4dmdmmlIHHjeIl3cXS7IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKF[HR1[tbY5lfWOnZDDj[YxtKG2rZ4LheIlwdg>? M2HGXVIyQTZ|M{C1
HUVEC MUPGeY5kfGmxbjDBd5NigQ>? NWiyPIRuOSEQvF2= NHftNWQyKGh? NIXFeo1KdmirYnn0bY9vKG:oIFXST{BxcG:|cHjvdplt[XSrb36gZZQhXGi{MkCyM3R6ejJyNDDpckBXTUeILYP0bY12dGG2ZXSgTHVXTUN? MY[yNVk3OzNyNR?=
HUVEC NUXl[pJsTnWwY4Tpc44hSXO|YYm= MoXXNUDPxE1? NF\CT48yKGh? M{m2[WlvcGmkaYTpc44hd2ZiZV7PV{BxcG:|cHjvdplt[XSrb36gZZQhW2W{LUGxO|IhcW5iVlXHSk1{fGmvdXzheIVlKEiXVlXD M376blIyQTZ|M{C1
HUVEC NWfOWnhyU2mwYYPlJGF{e2G7 MYixJO69VQ>? MVyxJIg> MnK5TY5pcWKrdHnvckBw\iCYRVfGVlIheGixc4Doc5J6dGG2aX;uJIF1KHS7cj2xNVc2KGmwIG\FS2Yue3SrbYXsZZRm\CCKVW\FRy=> NY[2UGtwOjF7NkOzNFU>
HUVEC MlyzSpVv[3Srb36gRZN{[Xl? NVHhN|NWOSEQvF2= NHrMOo8yKGh? MUfkc4V{KG6xdDDpcohq[mm2IFHLWEBxcG:|cHjvdplt[XSrb36gZZQhW2W{LUS3N{BqdiCYRVfGMZN1cW23bHH0[YQhUFWYRVO= MX[yNVk3OzNyNR?=
HL60 NYDsbFRSS3m2b4TvfIlkKEG|c3H5 NUDvWJBHPTBizszN MnyyOFghcA>? NVLLXGhZTE2VTx?= Ml;sTWM2OD1zNT61JO69VQ>? NFy3[WYzOjBzOUG4PC=>
K562 MorER5l1d3SxeHnjJGF{e2G7 M2rZXlUxKM7:TR?= M{jTflQ5KGh? MnX4SG1UVw>? NH6xZoZKSzVyPUKxMlkh|ryP M1S1Z|IzODF7MUi4
PC3 NVO3NFBsS3m2b4TvfIlkKEG|c3H5 NG\pfGM2OCEQvF2= NVH5blB3PDhiaB?= NUP2PZpWTE2VTx?= MnnFTWM2OD1{NT6xJO69VQ>? Mne4NlIxOTlzOEi=
SF-539 Mn:3T4lv[XOnIFHzd4F6 M3vGclM{OyEQvF2= M3LnNFYxKG2rbh?= MX3Jcohq[mm2aX;uJI9nKFCGR1\SZoV1[SC2eYLvd4lv\SCtaX7hd4Uh[WO2aY\peJkhcW5iUFTHSk1DSi2|dHnteYxifGWmIHj1cYFvKFOILUWzPUBk\WyuczD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> MX6yNlIxPDd2MR?=
HAEC NIPK[ldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSxNFAh|ryP MorQO|IhcA>? M{\lWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFHFR{Bk\WyuczDlfJBz\XO|aX7nJHZGT0[UIIfpeIghUUN3MDDv[kAxNjFizszN MkX5NlI1PDR4N{m=
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OVCAR3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGxNFAh|ryP MkPsOFghcA>? NYPCeo9MTE2VTx?= NIHZUXlIUTV|PUOuNkDPxE1? MWOyNlU3ODZ{Nx?=
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HT-29 MYjDfZRwfG:6aXOgRZN{[Xl? MlrENVAxKM7:TR?= MXm3NkBp NUnjepR3TE2VTx?= NXfObIZIS3m2b4TvfIlkcXS7IHHnZYlve3RiVlXHSnIh\XiycnXzd4lv\yCqdX3hckBJXC1{OTDj[YxteyC5aYToJGlEPTBib3[gNE4{OyEQvF2= Mnf1NlMyOzF3NEG=
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HUVEC MnTlSpVv[3Srb36gRZN{[Xl? MWiyJO69VQ>? NFzxdWsyQCCq Mn\iSG1UVw>? MonURY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliaX6gTHVXTUO|IIXu[IVzKGi7cH;4bYMh[2:wZHn0bY9vKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhfHWkZTDmc5Ju[XSrb36= MlK2NlMyPTN{MEC=
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MDA-MB-231 NV;1bWJES3m2b4TvfIlkKEG|c3H5 NVP2Vnh4PzJiaB?= M4rGSmROW09? NEGxSIhKSzVyPUCuNFIzOyEQvF2= NETweWEzPDh7ME[1Ni=>
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MDA-MB-468 NWXUb4tTS3m2b4TvfIlkKEG|c3H5 M3PVdFczKGh? M1T6PWROW09? NFT5cGRKSzVyPUCuNFA3OSEQvF2= MmjjNlQ5QTB4NUK=
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SH-SY5Y NFK5TGhMcW6jc3WgRZN{[Xl? MnjqNVAh|ryP MorGNUBp NYmyO2EzTE2VTx?= Mnn3TY5pcWKrdHnvckBw\iCSRFfGVoJmfGFid3n0bEBKSzVyIH;mJFAvODh|MTFOwG0> M1HSSlI1QDlyNkWy
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Bel7402 NHXnUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\hbnE4OiCq NGTv[5VFVVOR MYrJR|UxRTJwNkeg{txO MnH4NlQ6ODR7NkG=
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TT MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDoT|Y4OiCq NFnXcpVFVVOR NF7N[YNKSzVyPUCuNFQh|ryP MoC5NlQ6ODR7NkG=
EoL-1-cell M1;O[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jVT2lEPTB;MT62OEBxVQ>? M4HyVnNCVkeHUh?=
MV-4-11 MofZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITQT5VKSzVyPUK3NkBxVQ>? MoHhV2FPT0WU
NOS-1 MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF3LkOgcm0> MWLTRW5ITVJ?
CGTH-W-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf0TWM2OD1|MD65OEBvVQ>? MWTTRW5ITVJ?
MONO-MAC-6 NV;MNJZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzNRWhGUUN3ME2zN{45KG6P M1\lXXNCVkeHUh?=
ALL-PO NELqWYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\LTWM2OD15OT64PUBvVQ>? M2e5[nNCVkeHUh?=
NKM-1 NUmxSXl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTl6LkWyJI5O Mny1V2FPT0WU
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TE-15 NWDpNlk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTVyNz62NUBvVQ>? MUjTRW5ITVJ?
697 M2TDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C2OGlEPTB;NkG0MlI2KG6P MYLTRW5ITVJ?
MOLT-16 NFnYephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PINmlEPTB;NkOxMlMzKG6P MlW3V2FPT0WU
GB-1 NEPzNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkixTWM2OD15MUCuNlMhdk1? MUPTRW5ITVJ?
TE-12 MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnGxTWM2OD16MESuOVUhdk1? MYDTRW5ITVJ?
ES6 NVn1WlE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH5TWM2OD17OEGuNFYhdk1? NYDVZ4s1W0GQR1XS
LC-2-ad MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq5VIxzUUN3ME2xMlEyPDB5IN88US=> MkK5V2FPT0WU
BL-70 MoLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG3RVdWUUN3ME2xMlEyQDR4IN88US=> MWnTRW5ITVJ?
ETK-1 MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHv3cG5KSzVyPUGuNlg2QCEQvF2= MXnTRW5ITVJ?
A4-Fuk MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUCxV4FyUUN3ME2xMlM1OTRzIN88US=> NFHNcmJUSU6JRWK=
OCI-AML2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LlWWlEPTB;MT6zOlg2OSEQvF2= NGLpXJZUSU6JRWK=
SIG-M5 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPjTWM2OD1zLkO3NFA6KM7:TR?= MWnTRW5ITVJ?
NCI-SNU-16 M2nUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwNE[0PFYh|ryP NGH0OnBUSU6JRWK=
PSN1 Mlf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPKTWM2OD1zLkWwOlc3KM7:TR?= MX\TRW5ITVJ?
SR NF7LZ3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfvdYtIUUN3ME2xMlU1PTd{IN88US=> NYL3eoVqW0GQR1XS
A3-KAW M2jCfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nj[WlEPTB;MT62NlU1PiEQvF2= M3LjZ3NCVkeHUh?=
KS-1 MlHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{L1N2lEPTB;MT62PVI1PyEQvF2= MkfhV2FPT0WU
CTV-1 M{XoeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzuN5NKSzVyPUGuO|I4PTFizszN Mn;pV2FPT0WU
LB1047-RCC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTFwOEG2NlQh|ryP NWGwOGw1W0GQR1XS
EMG-01 M17NeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFwOEO1OlMh|ryP MV;TRW5ITVJ?
TE-11 MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwOEO5PFUh|ryP NE\HRZVUSU6JRWK=
CMK MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTFwOUW1NVch|ryP NHTHbFJUSU6JRWK=
NB1 M{GyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVryOoVzUUN3ME2xMlk3OTF5IN88US=> MYLTRW5ITVJ?
HAL-01 NIXpO|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;4PJdKUUN3ME2yMlA2QTR4IN88US=> MmXqV2FPT0WU
DEL M1vqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfmWINKSzVyPUKuNFg1QDJizszN MXfTRW5ITVJ?
RL95-2 NWL1Tok3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTVVlV4UUN3ME2yMlEyOTN5IN88US=> NInMdIdUSU6JRWK=
KARPAS-299 MmL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnTcFVqUUN3ME2yMlEyOzF|IN88US=> MXTTRW5ITVJ?
EW-16 NUT2XYJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fY[GlEPTB;Mj6xN|UxQCEQvF2= MXPTRW5ITVJ?
RS4-11 MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHPN2xGUUN3ME2yMlE4QTJ2IN88US=> M2fPVnNCVkeHUh?=
BB30-HNC NU\R[G9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTJwMkKzO|Uh|ryP NGTQUIlUSU6JRWK=
DOHH-2 NUGzTHVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVznXo5UUUN3ME2yMlM{PDNzIN88US=> MlTnV2FPT0WU
RPMI-8402 MmTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fsTWlEPTB;Mj6zN|YyQCEQvF2= NGLj[YRUSU6JRWK=
BV-173 MlXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJwM{O2OkDPxE1? MnnFV2FPT0WU
TE-10 NUToSZc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJwM{SzPFQh|ryP MXLTRW5ITVJ?
TE-8 M1fUXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrWUIF2UUN3ME2yMlM4ODN6IN88US=> NFKwU|VUSU6JRWK=
K052 M2[wZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TBSmlEPTB;Mj60NFIxOiEQvF2= MkO3V2FPT0WU
KARPAS-45 NHnNWZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjjd4pKSzVyPUKuOFk1PDZizszN MlLNV2FPT0WU
SK-NEP-1 NYnu[pFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e5VWlEPTB;Mj62NFI{PyEQvF2= NVT1NXBIW0GQR1XS
KGN NFe3V4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJwNkCzN|kh|ryP NUO3c4RFW0GQR1XS
ML-2 MkD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn4dZd{UUN3ME2yMlY{PTF{IN88US=> M2H6S3NCVkeHUh?=
LAMA-84 NFXlS4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlG3TWM2OD1{Lk[5OVQ2KM7:TR?= NXjKO2Q4W0GQR1XS
LXF-289 NG[wZ2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3CW|UxUUN3ME2yMlczQTh7IN88US=> M1q0U3NCVkeHUh?=
A101D MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jJOWlEPTB;Mj63PFMxPCEQvF2= MUPTRW5ITVJ?
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NALM-6 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\2U29vUUN3ME2yMlkxPDd|IN88US=> M1vGZXNCVkeHUh?=
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NCI-H209 M1n0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[yOJZ3UUN3ME24MlEyPjV{IN88US=> NVLDPI52W0GQR1XS
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SK-N-FI NW[3WHRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTF5Lk[5NVMh|ryP M33C[HNCVkeHUh?=
NTERA-S-cl-D1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvmTXFKSzVyPUG3Mlg2PzJizszN NXXM[Xl4W0GQR1XS
NCI-H1882 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1OwXmlEPTB;MUeuPVg{PCEQvF2= MmXKV2FPT0WU
A704 NE[0NG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTPV4g1UUN3ME2xO{46QTB2IN88US=> MUfTRW5ITVJ?
L-428 M2jjRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF6LkCxOVEh|ryP MV7TRW5ITVJ?
HCC1187 Mn;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3H1fmlEPTB;MUiuNFE5PyEQvF2= NX7CfohEW0GQR1XS
NCI-H1581 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\YbWlEPTB;MUiuNFg3PiEQvF2= MVrTRW5ITVJ?
BB65-RCC M1OwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF6LkSxOlIh|ryP MUTTRW5ITVJ?
EM-2 M{TTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHRTWM2OD1zOD61OlczKM7:TR?= NFHicHZUSU6JRWK=
Raji M1\MW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTF7Lkm1OlUh|ryP MofaV2FPT0WU
TE-1 M4PpdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjQUXB1UUN3ME2yNE41OTB2IN88US=> M{LZWHNCVkeHUh?=
SW962 M2HrR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTJyLkSyPVMh|ryP MX\TRW5ITVJ?
MHH-NB-11 NFvQOYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnqTWM2OD1{MD61OVIyKM7:TR?= NXrRbWF2W0GQR1XS
no-10 NIDS[INIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknpTWM2OD1{MT6wNlY1KM7:TR?= NFnyfWJUSU6JRWK=
GDM-1 NXi4U5NCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH5V4tiUUN3ME2yNU46PDF2IN88US=> M2DOT3NCVkeHUh?=
KMS-12-PE NHXoTJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mne2TWM2OD1{Mj6yO|Qh|ryP MXzTRW5ITVJ?
NCI-H510A NYXMe4w3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2npZWlEPTB;MkSuNVI4QCEQvF2= M1PIXXNCVkeHUh?=
ES5 M{XPVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ2LkezOFkh|ryP NX3ZVZFyW0GQR1XS
JiyoyeP-2003 MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzUN2tKSzVyPUK2MlI4PDJizszN NYfRSGRuW0GQR1XS
NMC-G1 NYDKb4RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJ5LkG4NlIh|ryP NYP6UlV3W0GQR1XS
NCI-H446 NULpdmVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TGVmlEPTB;MkeuOFk1PiEQvF2= MWTTRW5ITVJ?
NB7 M3fPfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITteVZKSzVyPUK3MlkzOjlizszN MUXTRW5ITVJ?
A388 M1\XUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPFSXVKSzVyPUK4MlAxPzRizszN MXrTRW5ITVJ?
JVM-2 Mnn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnv[ZB{UUN3ME2yPE4zQDl6IN88US=> M1PJUHNCVkeHUh?=
HT-144 M3nIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXXTWNxUUN3ME2yPE43QSEQvF2= NFvTZlVUSU6JRWK=
NCI-H747 M2HIRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJ6LkmxPVUh|ryP NG\Vem9USU6JRWK=
NCI-H1650 M4PlPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJ7LkCxO|Yh|ryP MnrEV2FPT0WU
EB-3 NXf5dHJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HOemlEPTB;MkmuOVMxQSEQvF2= NY\NOFJ5W0GQR1XS
KLE Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfZTWM2OD1{OT62NVkh|ryP MX;TRW5ITVJ?
TK10 M2m4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\KTWM2OD1|MD6xNlYh|ryP NWfpTXpZW0GQR1XS
COLO-668 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXUSoZXUUN3ME2zNE44QTJizszN NIixNolUSU6JRWK=
NCI-H23 NIf2NoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jlSWlEPTB;M{GuNVA3OyEQvF2= NYrpUWN4W0GQR1XS
GOTO MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;PS3JKSzVyPUOxMlYxQDVizszN NVTIZXVFW0GQR1XS
MSTO-211H MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTNzLki2O|gh|ryP NFvXPYRUSU6JRWK=
LB831-BLC NYrubHRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXp[|FiUUN3ME2zNk4{QDR|IN88US=> M2L1fnNCVkeHUh?=
SCH NEC1SGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm4[21sUUN3ME2zNk45PDh3IN88US=> NGjnZVRUSU6JRWK=
EHEB MnmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTN2LkGxPVMh|ryP MmPOV2FPT0WU
U-266 M1r2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[wT21jUUN3ME2zOE4zPzhzIN88US=> M4HCUHNCVkeHUh?=
EW-11 NUXYdGdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTtTWM2OD1|ND60O|I2KM7:TR?= NWXWXWxEW0GQR1XS
TE-9 M{fucGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTTTWM2OD1|Nz6wOFAyKM7:TR?= MWLTRW5ITVJ?
ES3 NFr4RolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHjTWM2OD1|Nz61NFA1KM7:TR?= MlXjV2FPT0WU
NCI-H2141 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTN6LkC4OFMh|ryP MljuV2FPT0WU
MPP-89 NEGxPJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml61TWM2OD12Mj6wOVg3KM7:TR?= NGS0TFlUSU6JRWK=
SK-MEL-2 NFz3b4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTR{Lk[0NFUh|ryP MnnFV2FPT0WU
LC-1F M4m2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTR|LkO2PFIh|ryP NVWycYZNW0GQR1XS
NH-12 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rYfWlEPTB;NEOuPVM2QSEQvF2= M{PLOHNCVkeHUh?=
RKO NEHIcJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPMTWM2OD12ND6xNlUzKM7:TR?= Ml;LV2FPT0WU
KM-H2 NX\i[otUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vkbGlEPTB;NESuPVU4PyEQvF2= M3rpVXNCVkeHUh?=
SK-UT-1 M{TkPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PWTGlEPTB;NEmuPFgzPSEQvF2= M2K4eHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:[1]
+ Expand

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:[3]
+ Expand
  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (28.16 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+ddH2O 2mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02761057 Recruiting Recurrent Renal Cell Carcinoma|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma National Cancer Institute (NCI) April 2016 Phase 2
NCT02779283 Recruiting Untreated Adult Acute Myeloid Leukemia OHSU Knight Cancer Institute|National Cancer Institute (NCI) December 2015 Phase 1
NCT02626754 Enrolling by invitation Renal Cell Carcinoma vghtpe user|Taipei Veterans General Hospital, Taiwan August 2015 Phase 2
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT01835158 Active, not recruiting Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) July 2013 Phase 2
NCT01740154 Terminated Fatigue|Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Case Comprehensive Cancer Center|National Cancer Institute (NCI) September 2012 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID